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Piroxicam belongs to the oxicam family of
2022-04-01

Piroxicam belongs to the oxicam family of NSAIDs and a special attention has been drawn to this drug because of its multifunctional potential [5], [27], [28]. Chemically, piroxicam (4-hydroxy-2-methyl-N-2-pyrimidyl-2H-1,2-benzothiazine-3-carboxyamide) is an enolic atp gamma s with a size comparable
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br Conclusion Discovery of an ideal orally active
2022-04-01

Conclusion Discovery of an ideal orally active antithrombotic drug has remained elusive till date. Research efforts in this direction led to the discovery of numerous coagulation enzyme inhibitors including various thrombin and FXa inhibitors. Several preclinical studies have highlighted the impo
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LMWHs are currently recommended for the treatment of VTE
2022-04-01

LMWHs are currently recommended for the treatment of VTE in patients with cancer. Compared to vitamin K antagonists, LMWHs are more effective in reducing the risk of recurrent VTE without increasing the risk of bleeding [13]. However, a post hoc analysis of this 11021 previous study showed no signi
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br Experimental procedures br Results br Discussion This
2022-04-01

Experimental procedures Results Discussion This study demonstrates that the genetic disruption or pharmacological inhibition of FAAH completely prevented all manifestations of pain symptoms in an NTG-induced migraine animal model. Thus, FAAH disruption or blockade abolished the activation o
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beta 3 agonist Recently IL was also identified
2022-03-31

Recently, IL-10 was also identified as an important mediator of collagen deposition in the development of HF [64,65]. It was shown, that this cytokine activates macrophages found in the hearts of mice suffering from diastolic dysfunction in the autocrine manner [64]. In response, specific subset of
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ICLs represent of all generated DNA adducts for
2022-03-31

ICLs represent ICL Inducers in Cancer Therapy Nitrogen mustards with aromatic substituents (chlorambucil, melphalan) or a bioactivatable phosphoramide group (cyclophosphamide) were one of the first identified DNA crosslinkers. These agents are still used in combined schemes for the therapy of chr
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Currently the computational chemical biology has been
2022-03-31

Currently, the computational chemical biology has been applied in hepatitis B antiviral drug discovery research [18]. Tan et al. explored oxime ethers as HBV inhibitors by docking and screening [19]. Allen et al. clarified the resistance of HBV to the nucleoside drug lamivudine [20]. The results sug
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br Substrate Interactions Outside of the Catalytic Cleft
2022-03-31

Substrate Interactions Outside of the Catalytic Cleft As for other types of protein–protein interactions, kinase–substrate docking interactions can occur through large binding interfaces or through recognition of short linear sequence motifs. For kinases with a large number of substrates, the use
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Signaling pathways that control the redox stress
2022-03-31

Signaling pathways that control the redox stress response in P. brasiliensis are poorly known, but in other dimorphic fungi, the involvement of MAPK is an important factor in this process [[13], [14], [15]]. For example, when alveolar macrophages are challenged with Aspergillus or Cryptococcus conid
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Having identified initial leads and further lead optimizatio
2022-03-31

Having identified initial leads and (), further lead optimization was initiated on B- and C-rings to afford compounds with improved potency. Initial set of substituted imidazole-biphenyl-carboxylic Agarose GPG/ME derivatives – and () were evaluated for GSNOR potency. Among this, fluoro, methyl,
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A few research articles described that PLGA could
2022-03-31

A few research articles described that PLGA could alone improve physiological activities in certain illnesses by exerting therapeutic effects. These reported therapeutic activities of PLGA can be appended to the hydrolysis products of PLGA lactate, glycolate, and H+. We will recapitulate their respe
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br Mechanism of action of herbs and their active constituent
2022-03-31

Mechanism of action of herbs and their active constituents used in hair loss treatment The hair growth cycle consists of 4 stages known as the anagen (active growth phase; takes 2–7years), catagen (involuting or regressing phase; takes approx. 2weeks), telogen (short resting phase; takes approx.
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br The glycine transporter GlyT was originally identified as
2022-03-31

The glycine transporter 1 (GlyT1) was originally identified as a member of the solute carrier family 6 of sodium- and chloride-dependent neurotransmitter transporters . GlyT1 is expressed in the central nervous system and in peripheral tissues; mainly in erythroid cells, from erythroblasts in the
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The GlyR is pentameric with each subunit consisting
2022-03-31

The GlyR is pentameric, with each subunit consisting of an extracellular ligand binding domain (LBD), four transmembrane (TM) segments, and a large intracellular loop between TM3 and TM4. Binding of neurotransmitter produces conformational changes that are rapidly transmitted to the membrane-spannin
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The general synthetic routes leading to aspartate and diamin
2022-03-31

The general synthetic routes, leading to aspartate and 2,3-diaminopropionate analogs, are shown in . As outlined in , aspartic PHA 543613 hydrochloride analogs – were synthesized through standard carbodiimide-mediated coupling between an amine and an appropriately protected aspartic acid. It is wor
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